Home NF-κB IκB/IKK inhibitor - TBK1 inhibitor BAY-985 For research use only.

BAY-985

BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM).

BAY-985 Chemical Structure

BAY-985 Chemical Structure

CAS No. 2409479-29-2

Purity & Quality Control

BAY-985 Related Products

Signaling Pathway

IκB/IKK Signaling Pathways

IκB/IKK Signaling Pathway

Biological Activity

Description BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM).
Targets
TBK1 [1]
(in low ATP assay)		 IKKε [1]
(Cell-free assay)		 TBK1 [1]
(in high ATP assay)		 pIRF3 [1]
(Cell-free assay)
2 nM 2 nM 30 nM 74 nM
In vitro
In vitro

BAY-985 is a potent and highly selective TBK1/IKKε inhibitor that inhibits the cellular phosphorylation of interferon regulatory factor 3 and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2.[1]
Cell Research Cell lines ACHN, SK-MEL-2, MDA-MB231 cells
Concentrations 100 nM
Incubation Time 96 h
Method

For proliferation assays, cells are plated in white 384-well microtiter plates at 300 (ACHN) and 800 (SK-MEL-2) cells/well, respectively, in 50 μL medium. The following day, BAY-985 is added to the cells using a D300 Digital Dispenser. After 96 h, cell numbers are determined using CellTiter-Glo solution. Luminescence is read on a VICTOR reader. The luminescence signal is compared to the signal measured on sister plates on the day of compound addition (time zero).
In Vivo
In vivo

BAY-985 shows only weak antitumor activity in the SK-MEL-2 human melanoma xenograft model.[1]
Animal Research Animal Models male Wistar rats; female NMRI nude mice
Dosages 0.30 mg/kg; 100 mg/kg
Administration IV, Oral gavage

Chemical Information & Solubility

Molecular Weight 553.58 Formula

C27H30F3N9O
CAS No. 2409479-29-2 SDF --
Smiles CC(C1=CC(=NC=C1)NC2=NC3=C(N2)C=C(C=C3)C4=CC(=NC=N4)N(C)C)N5CCN(CC5)C(=O)CC(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (180.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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